The Antihistaminic Drugs. A Review of the Literature

The purpose of this study was to determine the effects of subchronic exposure to the antihistamine pyrilamine maleate and to establish dosage levels to use in a 2-year chronic study. A 14-day repeated-dose study in male and female B6C3F1 mice at dietary levels of pyrilamine (as the free base) of 0, 196, 392, 783, 1563, or 3122 ppm revealed no influence on body weight gain and resulted in no deaths, nor abnormal clinical or gross necropsy observations. Parotid gland cell necrosis was more apparent in high-dosage groups than in controls of either gender. Male and female B6C3F1 mice also were administered pyrilamine for 90 days at dietary concentrations of 0, 375, 750, 1500, 3000, or 6000 ppm. Weight gain was markedly suppressed in the 6000 ppm group, but less so at 1500 and 3000 ppm. Parotid gland cell necrosis was apparent in males receiving 750 ppm pyrilamine and above and in females at 1500 ppm and above. Cytomegaly was noted in the parotid glands of both sexes at midlevel dosages but not in control, low-dosage, or high-dosage animals. It was concluded that 1500 ppm pyrilamine would not be life-threatening to B6C3F1 mice in a chronic study.

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“…The acute toxicity of pyrilamine was reviewed by Haley (1948). Pyrilamine maleate has an oral LD,, of 338 mgkg in mice.…”

Section: Introductionmentioning

confidence: 99%

“…The LD,, was 102 rndkg in mice when given intraperitonealIy (Lewis andTatken, 1980). Signs of acute toxicity of pyrilamine include Struab tail phenomenon, squeaking, restlessness, generalized tremor, increased activity, convulsions, and death by asphyxia (Haley, 1948).…”

Section: Introductionmentioning

confidence: 99%

Subchronic Studies of Pyrilamine in B6C3F₁ Mice

Greenman¹,

Morrissey²,

Gaylor³

et al. 1993

Journal of the American College of Toxicology

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“…The addition product afforded the starting sulfa compound after being worked up. The use of other nonpolar solvents such as carbon tetrachloride (6-S), absolute The present investigation, however, is coiicerned with tlir syiithesis of sutne phosphorus coiiipuuiids viu the condensation of phosphorus tricliloride with ether (2- 4,9), and dry benzene (2, 9) which were used by otlier investigators proved ullsuitdble because sulfanilamide itself is insoluble in these sol--.…”

Section: -Propionyloximino Benzoylthiophene (Xi1)-mentioning

confidence: 77%

“…Several attempts were made to condense sulfanilamide with phosphorus trichloride. Condensation in reagent dioxane according to the method of Cates (1,4) proved to be unsatisfactory due to the immediate formation of an insoluble addition complex which did not dissolve even when the reflux was continued for several hours. The addition product afforded the starting sulfa compound after being worked up.…”

Section: -Propionyloximino Benzoylthiophene (Xi1)-mentioning

confidence: 99%

Synthesis of ketoximino esters as antihistaminics

Lee

Williams

Kochhar³

1967

Journal of Pharmaceutical Sciences

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“…action between 929F and 15ilF and chioroauric acid would serve as additional evidence of their REFERENCES (1) Haley, T. I., THIS JOURNAL, 37, 378(1948).…”

mentioning

confidence: 99%